SU 14813

SU 14813 is a dual VEGFR and PDGFR family kinase inhibitor (IC50s = 0.002, 0.05, 0.004, and 0.015 µM for VEGFR1, VEGFR2, PDGFRbeta, and KIT, respectively). It is selective for these kinases over FGFR1, EGFR, Src, and c-Met (IC50s = 3.5, >20, 2.5, and 9 µM, respectively). SU 14813 inhibits VEGFR2, PDGFRbeta, KIT, and FLT3-internal tandem duplication (FLT3-ITD) phosphorylation in vitro (IC50s = 0.04, 0.02, 0.006, and 0.05 µM, respectively). It inhibits PDGF-dependent proliferation of NIH3T3 cells overexpressing PDGFRbeta, as well as OC1-AML5 cells expressing wild-type FLT3 and MV4-11 cells carrying the activating FLT3-ITD mutation. SU 14813 inhibits VEGF-induced survival of human umbilical vein endothelial cells (HUVECs, IC50 = 6.8 nM). It reduces tumor growth in human acute myeloid leukemia, renal, and colon cancer, as well as rat glioma, mouse xenograft models when used at doses ranging from 10 to 80 mg/kg twice per day.Formal Name: 5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-(4-morpholinyl)propyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide. CAS Number: 627908-92-3. Molecular Formula: C23H27FN4O4. Formula Weight: 442.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 0.1 mg/ml, PBS (pH 7.2): 0.1 mg/ml. lambdamax: 273, 428 nm. SMILES: O[C@H](CN1CCOCC1)CNC(C2=C(C)NC(/C=C3C4=CC(F)=CC=C4NC\3=O)=C2C)=O. InChi Code: InChI=1S/C23H27FN4O4/c1-13-20(10-18-17-9-15(24)3-4-19(17)27-22(18)30)26-14(2)21(13)23(31)25-11-16(29)12-28-5-7-32-8-6-28/h3-4,9-10,16,26,29H,5-8,11-12H2,1-2H3,(H,25,31)(H,27,30)/b18-10+/t16-/m0/s1. InChi Key: CTNPALGJUAXMMC-HKJBKDEOSA-N.